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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
4 Results for "
SAR405838
" in MedChemExpress (MCE) Product Catalog:
Products (4)
4 Results for "SAR405838" in MCE Product Catalog:
4
Target:
Research Areas:
SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a Ki of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity .
Cat. No.: HY-18986S
Synonyms: MI-77301-d10
Cat. No.: HY-181606
Research Areas:
Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is a dual MDM2 and α5β1 integrin modulator. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 acts as an antiproliferative agent, apoptosis inducer and cell cycle regulator, induces reactivation of p53 and upregulation of p21, redistributes glioblastoma cells from the G0/G1 phase to the G2/M phase, and enhances apoptosis. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is applicable to the research of glioblastoma .
Cat. No.: HY-L949
1279 compounds
Spirocyclic compounds, with rigid 3D structures, high Fsp³ and strong conformational restriction, are highly privileged scaffolds in small-molecule drug screening. They overcome drawbacks of planar aromatic compounds such as poor solubility, high off-target risks and weak druggability. Their orthogonal bicyclic geometry fits well into protein pockets, improving target affinity, subtype selectivity, metabolic stability and membrane permeability, making them ideal for hit identification against kinases, GPCRs, PPIs and other targets.
Spirocyclic scaffolds have been widely applied in oncology, antivirals, hypertension and CNS diseases, leading to many approved drugs and clinical candidates. SAR studies show that spiro-atom chirality, ring size and heteroatom substitution dominate bioactivity and selectivity, with the scaffold mainly serving as a conformational anchor. Azaspirocycles, spirooxindoles and spirosteranes target GPCRs, kinases, MDM2-p53 and PPIs. Approved drugs including irbesartan, spironolactone and rolapitant confirm their druggability, while revumenib and SAR405838 show promise against undruggable targets.
The MCE Spirocyclic Druglike Library contains over 1,000 diverse, stereospecific molecules selected by Lipinski’s rules. It covers privileged cores such as azaspirocycles, oxaspirocycles and spirooxindoles. These molecules bear rich chiral centers and distinct 3D orientations, reducing non-specific binding and enhancing screening efficiency. Featuring novel scaffolds, the library offers a highly innovative starting point for drug discovery.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
